专利号:US-9353057-B2 优先权日:2003-12-30 标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof 发明人:GALLOP MARK A; DAI XUEDONG; SCHEUERMAN RANDALL A; RAILLARD STEPHEN P; MANTHATI SURESH K; YAO FENMEI; PHAN THU; LUDWIKOW MARIA; PENG GE; BHAT SEEMA 权利人:XENOPORT INC 摘要:Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.
专利号:US-5204456-A 优先权日:1986-04-08 标题:Derivatives of nucleosides and their use for the synthesis of oligonucleotides 发明人:MOLKO DIDIER; SCHULHOF JEAN-CLAUDE; TEOULE ROBERT 权利人:COMMISSARIAT ENERGIE ATOMIQUE 摘要:The invention relates to derivatives of nucleosides and their use for the synthesis of oligonucleotides. These derivatives are in accordance with the formula: (I) in which B represents a radical derived from guanine, cytosine or adenine, whose exocylic NH group is protected by the group with R1 representing a hydrogen atom or a alkyl radical and R2 a hydrogen atom, and alkyl radical, an alkoxy radical and optionally substituted aryloxy radical, R3 represents a hydrogen atom, the dimethoxytrityl radical or the radical R4 represents a hydrogen atom, the radical of formula: or a radical suitable for the synthesis of polynucelotides and R5 represents a hydrogen atom or the protected or unprotected hydroxyl OH radical.
专利号:US-2024317784-A1 优先权日:2021-07-13 标题 :Process for the synthesis of 4-((r)-2-{[6-((s)-3-methoxy-pyrrolidin-1-yl)-2-phenyl-pyrimidine-4-carbonyl]-amino}-3-phosphono-propionyl)-piperazine-1-carboxylic acid butyl ester 发明人:BLUMER NICOLE; CLAVEAU ROMAIN; FEYEN FABIAN; HALL LEANNE; HUGHES STEPHEN; REBER STEFAN 权利人:VIATRIS ASIA PACIFIC PTE LTD 摘要:The present invention relates to a process for the synthesis of 4-((R)-2-{[6-((S)-3-methoxy-pyrrolidin-1-yl)-2-phenyl-pyrimidine-4-carbonyl]-amino}-3-phosphono-propionyl)-piperazine-1-carboxylic acid butyl ester, or of a hydrochloride salt thereof; and to a crystalline form of 4-((R)-2-{[6-((S)-3-methoxy-pyrrolidin-1-yl)-2-phenyl-pyrimidine-4-carbonyl]-amino}-3-phosphono-propionyl)-piperazine-1-carboxylic acid butyl ester hydrochloride.
专利号:EP-1085020-B1 优先权日:1999-09-17 标题 :Synthesis of peptide nucleic acids 发明人:BATZ HANS-GEORG; HANSEN HENRIK FRYDENLUND; OERUM HENRIK; KOCH TROELS; KOFOED THOMAS 权利人:PNA DIAGNOSTICS APS APPLIED BI 摘要:Protected diaminopurines can be used in the synthesis of nucleic acid binding compounds containing diaminepurine in place of other nucleobases. A method for the synthesis of protected diaminopurines is disclosed which is convenient for incorporating modified diaminopurines into monomers or into oligomers for the preparation of nucleic acid binding compounds.
专利号:US-2023287032-A1 优先权日:2020-08-14 标 题:Synthesis of fluorinated nucleotides 发明人:CHUNG CHEOL KEUN; LIU ZHIJIAN; MALIGRES PETER E; MAO EDNA; OBLIGACION JENNIFER V; PHILLIPS ERIC M; PIRNOT MICHAEL; POIRIER MARC; SONG ZHIGUO JAKE; WANG TAO 权利人:CHUNG CHEOL KEUN; LIU ZHIJIAN; MALIGRES PETER E; MAO EDNA; OBLIGACION JENNIFER V; PHILLIPS ERIC M; PIRNOT MICHAEL; POIRIER MARC; SONG ZHIGUO JAKE; WANG TAO; MERCK SHARP & DOHME LLC 摘要:The present invention relates to efficient processes useful in the preparation of fluorinated nucleosides, such as (O—{[(2R,3R,4S,5R)-5-(6-amino-9H-purin-9-yl)-4-fluoro-3-hydroxyoxolan-2-yl]methyl}O,O-dihydrogen phosphorothioate, also known as 2′-(S)-fluoro-thio-adenosine monophosphate or 2′-F-thio-AMP. Such fluorinated nucleosides may be useful as a biologically active compound and or as an intermediate for the synthesis of more complex biologically active compounds. The present invention also encompasses intermediates useful in the disclosed synthetic processes and the methods of their preparation.
专利号:US-7273933-B1 优先权日:1998-02-26 标 题 :Methods for synthesis of oligonucleotides 发明人:KROTZ ACHIM H; RAVIKUMAR VASULINGA T 权利人:ISIS PHARMACEUTICALS INC 摘要:Improved methods for synthesis of oligonucleotides and other phosphorus-linked oligomers are disclosed. The methods include the use of aromatic solvents, alkyl aromatic solvents, halogenated aromatic solvents, halogenated alkyl aromatic solvents, or aromatic ether solvents to achieve deprotection of protected hydroxyl groups.
摘要:Wang, K. K., Science of Synthesis, (2008) 44, 259. 摘要:Wyatt, P. B., Science of Synthesis Knowledge Updates, (2014) 4, 3. 摘要:Davies, G. H. M.; Wisniewski, S. R., Science of Synthesis Knowledge Updates, (2021) 2, 121. 摘要:Lubell, W. D.; St-Cyr, D. J.; Dufour-Gallant, J.; Hopewell, R.; Boutard, N.; Kassem, T.; Dörr, A.; Zelli, R., Science of Synthesis Knowledge Updates, (2013) 1, 177. 摘要:Joule, J. A., Science of Synthesis Knowledge Updates, (2010) 2, 293.